Stereoselective enhancement by (R)-HA-966 of the binding of [3H]CPP to the NMDA receptor complex
| Autor: | Robert J. Stumpo, Maryann Britt, Andrea B. Klika, B.A. Meiners, Andre I. Salama, Linda M. Pullan, Richard J. Powell |
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| Rok vydání: | 1990 |
| Předmět: |
Pharmacology
Stereochemistry Antagonist Glutamate receptor Synaptic Membranes Spermine Rats Inbred Strains Stereoisomerism Strychnine Biology In Vitro Techniques Kynurenic Acid Receptors N-Methyl-D-Aspartate Piperazines Pyrrolidinones Rats chemistry.chemical_compound chemistry Competitive antagonist Glycine NMDA receptor Animals HA-966 Polyamine |
| Zdroj: | European journal of pharmacology. 189(2-3) |
| ISSN: | 0014-2999 |
| Popis: | The enantiomers of the strychnine-insensitive glycine antagonist, HA-966 (1-hydroxy-3-amino-pyrrolidone-2), stereoselectively enhance binding of the N-methyl-D-aspartate (NMDA) competitive antagonist, [3H]CPP (3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid) to rat brain synaptosomal membranes. The enhancement by the more potent (R)-HA-966 is competitively inhibited by the glycine antagonist 7-chlorokynurenic acid and noncompetitively by the polyamine spermine. Thus, (R)-HA-966, apparently at the glycine site, enhances the binding of antagonist to the NMDA receptor, possibly through a mechanism partially in common with that of spermine. |
| Databáze: | OpenAIRE |
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